title: Synthesis and inhibitory effects of some novel 1,3-diarylprop-2-en-1-one analogues in Foxp3 expression: a novel class of anti-cancer candidates.
abstract: A series of novel analogues of 1,3-diarylprop-2-en-1-one (3a-m) were synthesized and evaluated for their inhibitory activity of FOX P3 gene expression and apoptosis in CD4(+)T cells that had been isolated from the spleen of 8 to 10 weeks old mice. The structure-activity relationship (SAR) of the R1 and R2 modification was studied to identify a candidate with the maximum potency. Of these compounds, 3d showed the highest inhibitory activity of FOX P3 gene expression and apoptosis (66.5 % inhibition at 10 μM). To the best of the authors' knowledge this is the first report of 1,3- diarylprop-2-en-1-ones as regulators of FOX P3 gene expression.
authors.affiliation: Department of Advanced Materials Chemistry, College of Science and Technology, Dongguk University-Gyeongju, 780-714, Republic of Korea. swkim@dongguk.ac.kr.
authors.forename: Mayank
authors.initials: M
authors.lastname: Kinger
authors.forename: Jeong Hoon
authors.initials: JH
authors.lastname: Park
authors.forename: Min Goo
authors.initials: MG
authors.lastname: Hur
authors.forename: Sang Wook
authors.initials: SW
authors.lastname: Kim
authors.forename: Seung Dae
authors.initials: SD
authors.lastname: Yang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000145:classification* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D015496:CD4-Positive T-Lymphocytes / Q000187:drug effects; D002454:Cell Differentiation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D051858:Forkhead Transcription Factors / Q000235:genetics*; D005786:Gene Expression Regulation / Q000187:drug effects* / Q000235:genetics; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011427:Propiophenones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013154:Spleen / Q000166:cytology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D051858:Forkhead Transcription Factors; C498833:Foxp3 protein, mouse; D011427:Propiophenones; D011720:Pyrazoles